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TOSHIKAZU OKI, YASUE MATSUZAWA, KOHKI KIYOSHIMA, AKIHIRO YOSHIMOTO, HI ...
1981 Volume 34 Issue 7 Pages
783-790
Published: 1981
Released on J-STAGE: April 12, 2006
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Various blocked mutants were isolated from Streptomyces coendeorubidus ME130-A4 by NTG and UV treatments. Among them, mutant strain 4N-140 produced new anthracycline feudomycins A and B having new aglycones in which the side chain at C-9 position of daunomycinone was ethyl and acetonyl, respectively. New aglycones feudomycinones C and D having methyl at C-9 and additional hydroxyl group at C-10 of daunomycinone were also isolated from this strain.
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WEN-CHIN Liu, SUSAN M. FISHER, J. Jr. SCOTT WELLS, CAROLYN S. RICCA, P ...
1981 Volume 34 Issue 7 Pages
791-799
Published: 1981
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A new ferrous-ion chelating agent, siderochelin, was isolated from fermentation broths of Nocardia sp. SC 11, 340. Siderochelin was produced by conventional submerged culture and purified by solvent extraction and recrystallization. The antibiotic was crystallized from acetonitrile as a mixture of diastereoisomers. The molecular formula of siderochelin was determined as C11H13N303 on the basis of elemental analysis and mass spectrometry, and the structure was elucidated by X-ray crystallography. The compound shows a broad spectrum of antimicrobial activity, being active against bacteria, fungi and protozoa.
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PREPARATION. CHEMICAL STRUCTURES AND BIOLOGICAL PROPERTIES OF HALF-ESTERS OF THE PEPTIDE ANTIBIOTIC
KATSUYA TOKURA, KUNIO HAYASHI, KEI OKABE, KAZUO TORI, YOHKO YOSHIMURA, ...
1981 Volume 34 Issue 7 Pages
800-810
Published: 1981
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The peptide antibiotic siomycin-A was transformed into half-esters with dicarboxylic acids with the intention of making siomycin-A soluble in water. Sodium salts of the half-esters were also prepared. Some of the salts showed antibacterial activities comparable to siomycin-A against Gram-positive bacteria in vitro and exhibited better therapeutic effects in infected mice than siomycin-A. The chemical structures of siomycin-A hemiadipate-II and -III were elucidated by comparing their 13C and 1H NMR spectra with those of siomycin-A. Their physicochemical properties are described.
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IV. SPORARICINS C AND D
TAKEO DEUSHI, ISAMU WATANABE, AKIO IWASAKI, KAZUHIRO KAMIYA, TOSHIMI M ...
1981 Volume 34 Issue 7 Pages
811-817
Published: 1981
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Two new aminoglycoside antibiotics, sporaricins C and D have been isolated from the culture broth of Saccharopolyspora hirsuta subsp. kobensis, which produced sporaricins A and B. The structures of sporaricins C and D have been determined to be 4-N-carbamoylglycylsporaricin B and 4-N-formylglycylsporaricin B, respectively. Sporaricins C and D are active against Gram-positive and Gram-negative bacteria including aminoglycosideresistant strains.
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MASAHITO NAKAYAMA, SHIGERU KIMURA, SOHEI TANABE, TOSHIMI MIZOGUCHI, IS ...
1981 Volume 34 Issue 7 Pages
818-823
Published: 1981
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The structures and stereochemistries of carpetimycins A (
1) and B (
2) have been determined as shown below.
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HIROKAZU YAMAMOTO, KUNIMOTO HOTTA, YOSHIRO OKAMI, HAMAO UMEZAWA
1981 Volume 34 Issue 7 Pages
824-829
Published: 1981
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Streptomyces tenjimariensis SS-939, a producer of istamycins, is highly resistant to its own antibiotics and grows in Tryptic Soy Broth containing istamycin A or B at 3, 000 μg/ml. No istamycin-inactivating enzyme was detected in extracts of strain SS-939. Polyphenylalanine synthesis in an
in vitro system, consisting of the S-150 fraction and ribosomes prepared from strain SS-939, was not inhibited by 200 μg/ml of istamycins. Using reciprocally reconstituted systems consisting of S-150 fractions and ribosomes from strain SS-939 and those from
Streptomyces griseus ISP5236 (istamycin-sensitive strain), ribosomes of strain SS-939 were found to be resistant to istamycins. Thus, ribosomes have the main role in the self-resistance mechanism of
S. tenjimariensis SS-939.
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CRAIG S. ROTHROCK, DAVID GOTTLIEB
1981 Volume 34 Issue 7 Pages
830-835
Published: 1981
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Antagonism of ten
Streptomyces spp., five of which produce antibiotics, to the plant pathogens
Rhizoctonia solani and
Phytophthora megasperma var.
sojae was studied. Antibiotic activity was detected in culture for the five antibiotic producers.
S. griseus,
S. hygroscopicus var.
geldanus, and
S. noursei produced wide zones of inhibition to
R. solani and
P. megasperma var.
sojae. Similar activity was found for
S. reticuli var.
protomycicus to
P. megasperma var.
sojae.
S. cellulosae reduced Rhizoctonia root rot on pea when sterile soil was infested simultaneously with the antagonist and
R. solani.
S. hygroscopicus gave almost complete disease control when the streptomycete was added 7 days prior to infesting the soil with
R. solani. Several of the
Streptomyces spp. reduced Phytophthora root rot on soybean when the streptomycetes were added to soil at the same time as
P. megasperma var.
sojae or 7 days prior to adding the pathogen.
S. herbaricolor and
S. coeruleofuscus gave the most consistent control. No relationship was found between reported antibiotic activity or antagonism on agar media and reduction in disease severity. Only
S. hygroscopicus var.
geldanus gave both control of Rhizoctonia root rot and large zones of inhibition on agar media when the streptomycetes were preincubated in soil for 7 days.
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III. USE OF ULTRA HIGH PERFORMANCE COLUMNS AND ION-PAIRING TECHNIQUES
E. RODERICK WHITE, JOHN E. ZAREMBO
1981 Volume 34 Issue 7 Pages
836-844
Published: 1981
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Improved methods for the separation and quantitation of cephalosporin, penicillin, aminoglycoside and anthracycline antibiotics are presented. The use of ultra high performance 5 μm reverse phase columns combined with the added dimension of ion-pairing greatly increases the ease of separation and speed of analysis of complex antibiotic mixtures. Antibiotics in a variety of dosage forms and in fermentation broths have been examined in order to provide the maximum data on impurities to meet regulatory requirements for drug safety, purity and efficacy. Mixtures of antibiotics have been analyzed to demonstrate the improved separations, increased efficiency and shortened analysis times possible with ultra high performance columns. Under these improved conditions, the danger of multiple components in a single peak are markedly reduced.
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TAKESHI KUSAMA, AKIRA OKADA, MASAJI SEZAKI
1981 Volume 34 Issue 7 Pages
845-849
Published: 1981
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A high performance liquid chromatographic method for quantitative determination of neothramycin in plasma was developed. The procedure involves pretreatments for the removal of endogenous materials in plasma samples and separation on a reversed phase column. The antibiotic was monitored with a fluorescence detector and confirmed by a specific sulfite adduct shift of retention time. A linear response for serum samples containing neothramycin ranging from 50 to 500 ng/ml was obtained. The sensitivity of this method was sufficient to measure neothramycin in human plasma for 120 minutes after a 24 mg/m2 (body surface area) intravenous injection.
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4"'-AMINO, 4"'-ALKYLAMINO AND 4"'-AMIDE DERIVATIVES OF ACLACINOMYCIN A
HIROSHI TANAKA, TAKEO YOSHIOKA, YASUTAKA SHIMAUCHI, TOSHIKAZU OKI, TAI ...
1981 Volume 34 Issue 7 Pages
850-855
Published: 1981
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(4"'R)- and (4"'S)-4"'-Deoxo-4"'-aminoaclacinomycin A were derived by the reductive amination of aclacinomycin A, and further modified to 4"'-alkylamino and 4"'-amide derivatives by reductive
N-alkylation and acylation.
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TOSHIO NISHIMURA, JUNICHIRO KITAJIMA, SADAFUMI OMURA, NOBUO TANAKA
1981 Volume 34 Issue 7 Pages
856-861
Published: 1981
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An antibiotic, identical with or closely related to xanthomycin A, was isolated from a soil
Streptomyces. The antibiotic displayed significant therapeutic activity by i.p. administration against i.p.-implanted mouse tumors: Ehrlich carcinoma, sarcoma 180 and P388 leukemia. Less therapeutic activity was observed by i.p. injection in mice bearing s.c. solid tumors of Ehrlich carcinoma and sarcoma 180. No significant activity was found against L1210 leukemia, B16 melanoma and Lewis lung carcinoma.
In vitro the antibiotic exhibited a potent cytotoxicity to human leukemia K562 and mouse lymphoblastoma L5178Y cells. DNA strand scission of PM2 phage was caused by the antibiotic in the presence of dithiothreitol.
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T. H. HASKEL, P. W. K. WOO, E. D. NICOLAIDES, M. P. HUTT, G. G. HUANG, ...
1981 Volume 34 Issue 7 Pages
862-868
Published: 1981
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The synthesis and biological activities of a series of 12 new semisynthetic penicillins is described. These compounds consisted of acylated amino acid analogs of 6-substituted-1, 2-dihydro-2-oxonicotinic acid and 2-substituted-3, 4-dihydro-4-oxo-5-pyrimidinecarboxylic acid attached to amoxicillin. The effect of the amino acid substituent, chirality of amino acid and acyl function on biological properties is discussed.
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SHOJI SHIMIZU, MATSUHISA INOUE, SUSUMU MITSUHASHI, HIROSHI NAGANAWA, S ...
1981 Volume 34 Issue 7 Pages
869-875
Published: 1981
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Spectinomycin (SPC) was inactivated in the presence of adenosine-5'-triphosphate and magnesium ion by an enzyme preparation made from
Acinetobacter calcoaceticus subsp. anitratus GN12313 resistant to both SPC and streptomycin. The structure of the inactivated SPC was found to be the adenylylated product of the hydroxy group on C-9 of the actinamine moiety.
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YOSHIKO YOKOTA, TAKEO MURAKAWA, MINORU NISHIDA
1981 Volume 34 Issue 7 Pages
876-883
Published: 1981
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Against most test strains of Gram-negative bacilli, the
in vitro effect of FR-31564 together with β-lactam antibiotics or trimethoprim was strongly synergistic; with tetracycline and nalidixic acid the effect was additive; and with gentamicin and sulfamethoxazole the effect was additive or antagonistic. FR-31564 was markedly synergistic with β-lactam antibiotics against β-lactam antibiotic-resistant Gram-negative bacilli such as
Klebsiella pnemnoniae, Enterobacter aerogenes, E. cloacae, Citrobacter freundii and
Serratia marcescens. The combination of FR-31564 with β-lactam antibiotics effected a reduction of MICs against most of the test strains to clinically achievable concentrations in human serum.
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B. CYBULSKA, E. BOROWSKI, Y. PRIGENT, C. M. GARY-BOBO
1981 Volume 34 Issue 7 Pages
884-891
Published: 1981
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The cationic permeability induced by two aromatic heptaenes, vacidin A and candicidin D, has been studied on egg yolk L-α-phosphatidylcholine single walled vesicles as a function of cholesterol and ergosterol concentration. For comparison amphotericin B and nystatin were also tested. Vacidin A and candicidin D elicit cation permeability in both types of vesicles in the same concentration ranges and exhibit only quantitative differences in cholesterol and ergo-sterol vesicles. The active concentration range is of the same order of magnitude as the active concentration range of amphotericin B, at variance with what is obtained on biological cells. This difference is interpreted in term of mechanism of action of polyene on both biological and model membranes.
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YOKO TANAKA
1981 Volume 34 Issue 7 Pages
892-897
Published: 1981
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The effects of habekacin on corneal ulceration, caused by
Pseudonnonas aeruginosa IFO 3455, were studied in mice, in comparison with gentamicin and tobramycin. The minimal inhibitory concentrations of the antibiotics for the organism were: habekacin 2 μg/ml, genta-micin 2μg/ml, and tobramycin 1 μg/ml. Habekacin showed protective and therapeutic effects on
Pseudomonas keratitis. The 50% effective dose was approximately 1 μg per mouse, when the drug was topically applied three hours after the infection, and about 0.2 mg per mouse, when the antibiotic was intramuscularly injected one hour after the bacteria] chall enge to the cornea. Significant therapeutic and protective activities of habekacin were observed even by starting the topical and/or intramuscular treatment after the corneal ulcers were formed:
i.e. 15 hours after the bacterial infection. Complete cure of
Pseudonzonas keratitis was found within a week in a number of the infected mice by both topical and systemic administrations of the drug. The protective and therapeutic effects of habekacin were comparable to those of gentamicin and tobramycin.
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MONG-BING LIU, REBECCA BLACKSTOCK, RICHARD M. HYDE
1981 Volume 34 Issue 7 Pages
898-901
Published: 1981
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The aminoglycoside antibiotic, gentamicin, was conjugated to erythrocytes or bovine serum albumin (BSA) by a simple procedure in which ECDI was employed as the coupling reagent. When rabbits were immunized by injecting gentamicin-goat erythrocyte conjugates, three kinds of antibody were produced: 1. anti-gentamicin antibody, 2. anti-ECDI antibody, 3. goat erythrocyte agglutinins. The interfering anti-ECDI antibody was easily neutralized by adding acidified LCDI solution to the immune serum. Goat agglutinins were avoided by employing rabbit erythrocytes as the carrier cell in the hemagglutination titration. Highly specific anti-gentamicin antiserum was produced in rabbits by first injecting an initial dose of gentamicin-BSA conjugate as an emulsion in incomplete Freund's adjuvant
via the foot pad, followed by multiple intravenous injections of gentamicin-erythrocyte conjugates. The immunization took approximately 21 days. High titered anti-gentamicin antibody was also produced by foot pad inoculation of gentamicin-BSA conjugates; however, the time necessary to achieve comparable titers was considerably longer (55 days). The antibodies produced by both immunization procedures were mainly of the IgG class.
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V. P. MARSHALL, M. S. LITTLE, L. E. JOHNSON
1981 Volume 34 Issue 7 Pages
902-904
Published: 1981
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HIROSHI TANAKA, TAKEO YOSHIOKA, YASUTAKA SHIMAUCHI, YOSHIYUKI MATSUSHI ...
1981 Volume 34 Issue 7 Pages
905-908
Published: 1981
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KENTARO TANAKA, JUN'ICHI SHOJI, YOSHIHIRO TERUI, NAOKI TSUJI, EIJI KON ...
1981 Volume 34 Issue 7 Pages
909-911
Published: 1981
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AKIKO FUJIWARA, MASAAKI TAZOE, TATSUO HOSHINO, YUZURU SEKINE, SETSUKO ...
1981 Volume 34 Issue 7 Pages
912-915
Published: 1981
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TOSHIKAZU OKI, AKIHIRO YOSHIMOTO, YASUE MATSUZAWA, TOMIO TAKEUCHI, TOM ...
1981 Volume 34 Issue 7 Pages
916-918
Published: 1981
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DIFFERENOL A, A DIFFERENTIATION INDUCING SUBSTANCE AGAINST MOUSE LEUKEMIA CELLS
KEN-ICHI ASAHI, ICHIE ONO, HIROO KUSAKABE, GOTO NAKAMURA, KIYOSHI ISON ...
1981 Volume 34 Issue 7 Pages
919-920
Published: 1981
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YOSHIYUKI KAWAKAMI, KAZUO YAMASAKI, SHOSHIRO NAKAMURA
1981 Volume 34 Issue 7 Pages
921-922
Published: 1981
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